Estimating Binding Capability of Radiopharmaceuticals by Cell Culture Studies

Özdemir, Denis; Ekinci, Meliha; Gündoğdu, Evren; Aşıkoğlu, Makbule

doi:10.23937/2378-3664/1410014

Cited by 5 publications

(5 citation statements)

References 29 publications

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“…Also, some of them were excluded because of their particle size that is above 100 nm. According to results, formulation 7,8,10,11,14,17,18,19,20 were used for further studies.…”

Section: Particle Size Zeta Potential and Polydispersity Indexmentioning

confidence: 99%

“…Eight formulations which have below 100 nm of particle size ( Formulations 7,8,10,11,14,17,19,20) were selected for cytotoxicity studies. While F-17 shows 95.55%, 95.12%, 94.34% cell viability for MCF-7, CRL-10742, PCS-440-010 respectively, other formulations produce between 70.56% and 89.13% cell viability for all cells (Table 7).…”

Section: Cytotoxicity Studiesmentioning

confidence: 99%

“…The cytotoxicity of developed LPNs ( Formulation 7,8,10,11,14,17,18,19,20) was determined by the 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-tetrazolium bromide (MTT) assay. MCF-7, PCS-440-010 and CRL-10742 cells were plated in 0.1 mL of medium/well in 96-well plates (Costar Corning, Rochester, NY).…”

Section: Cytotoxicity Studiesmentioning

confidence: 99%

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Development and radiolabeling of lipid nanoparticles with [99mTc]Tc-HMPAO: Characterization, stability, cytotoxicity and cell binding studies

Gündoğdu¹,

ÖZGENÇ²,

Demir³

et al. 2022

jrp

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In this study, we aimed to develop new lipid based nanoparticles (LPNs) and radiolabeled LPNs with [ 99m Tc]Tc-HMPAO to investigate its cell binding capacity comparatively with [ 99m Tc]Tc-HMPAO on different cancer cells. According to obtained results, LPNs with zeta potential of -27.4 ± 0.95 mV, particle size of 93.5 ± 1.17 nm, and polydispersity index of 0.35 ± 0.04 were successfully developed. The optimum radiolabeling efficiency was found to be above 90% at 15-min of incubation time. The cell binding capacity of [ 99m Tc]Tc-HMPAO-LPNs was found to be higher than [ 99m Tc]Tc-HMPAO in cancer cell lines. The results demonstrated that [ 99m Tc]Tc-HMPAO-LPNs may be a promising agent for cancer diagnosis alternatively to [ 99m Tc]Tc-HMPAO.

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“…Also, some of them were excluded because of their particle size that is above 100 nm. According to results, formulation 7,8,10,11,14,17,18,19,20 were used for further studies.…”

Section: Particle Size Zeta Potential and Polydispersity Indexmentioning

confidence: 99%

Section: Cytotoxicity Studiesmentioning

confidence: 99%

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Development and radiolabeling of lipid nanoparticles with [99mTc]Tc-HMPAO: Characterization, stability, cytotoxicity and cell binding studies

Gündoğdu¹,

ÖZGENÇ²,

Demir³

et al. 2022

jrp

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“…Radiopharmaceuticals are drugs containing radioisotopes that are safe to administer to humans for diagnosis or therapy. The use of radiopharmaceuticals for imaging organ function and disease states is a unique capability in nuclear medicine 5 . Radionuclides or radioisotopes are atoms that have excess nuclear energy, making them unstable.…”

Section: Introductionmentioning

confidence: 99%

Radiolabeling and In-Silico Study of 131I-(4-fluorobenzoyl-3-methylthiourea) as Radiopharmaceuticals for Breast Cancer Theranostics

Pratama,

Ruswanto,

Nofianti

et al. 2024

Valensi

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The chemicals produced from thiourea are actively being studied as anticancer possibilities. In complexes with radionuclides like Iodine-131, the 1-(4-Fluorobenzoyl)-3-methyl thiourea is a promising ligand for theragnostic applications. This study aimed to label 1-(4-fluorobenzoyl-3-methylthiourea) with iodine-131 and observe its interaction with breast cancer receptors. The radiolabeling of 131I-(4-fluorobenzoyl-3-methylthiourea) uses the radioiodination method with Chloramine-T, and an in-silico investigation of breast cancer receptors was conducted. According to the results of molecular docking using AutoDockTools, this radiopharmaceutical molecule has the best activity on the HER2 receptor (PDB ID: 3PP0) compared to the native ligand and control positive, with a binding affinity of -6.13 kcal/mol and a Ki value of 32.05 mM. According to the molecular dynamics data using Desmond, the radiopharmaceutical molecule 131I-(4-Fluorobenzoyl-3-methylthiourea) displays good stability starting from the 50ns range. The indirect radioiodination method has successfully labeled 1-(4-Fluorobenzoyl-3-methylthiourea) with iodine-131.

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“…The mapping of the radiopharmaceutical distribution in vivo provides images of functional morphology of organs in a noninvasive manner and plays an important role in the diagnosis of many common diseases associated with the malfunctioning of organs in the body as well as in the detection of certain type of cancers. 5 A radionuclide (radioactive nuclide, radioisotope or radioactive isotope) is an atom that has excess nuclear energy, making it unstable. This excess energy can be used in one of three ways: emitted from the nucleus as gamma (γ) radiation; transferred to one of its electrons to release it as a conversion electron; or used to create and emit a new particle (alpha (α) particle or beta (β) particle) from the nucleus.…”

Section: Introductionmentioning

confidence: 99%

Labeling of Piperine with Iodine-131 as Radiotracer in the Development of Cancer Drugs from Indonesia’s Natural Products

Daruwati¹,

Anggraini²,

Wangsaatmadja³

2019

IJPST

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Piperine, as one of the secondary metabolites of pepper, shows many pharmacological activities in various studies, including as antiinflammatory, antimicrobial, hepatoprotective, antioxidant, and potentially anticancer agents. Cancer is still one of the leading causes of death in the world due to the absence of specific symptoms in early-stage of cancer. The development of drugs for early diagnosis and selective treatment of cancer cells is considered one of the best solutions to reduce mortality. The activity of piperine that could induce apoptosis of 4T1 breast cancer cells and HT-29 colon cancer cells at in vivo trials prove it as a potential compound that can carry radioactive atoms (as labeledcompound) to cancer cells. This study was conducted to determine the optimal conditions of labeling of piperine with iodine-131 in order to obtain a 131 I-piperine which can later be used as a radiotracer in the development of cancer drugs. The labeling of piperine was performed by Chloramine-T iodination method and followed by purification with ion exchange chromatography. The optimal labeling results of piperine with 43.99% ± 1.23 radiochemical purity were obtained with piperine 3mg/300μL, chloramine-T 50 μg as an oxidizer, incubation time 30 min at room temperature, and 100 μg sodium metabisulphite as a reductor. To improve the purity of the preparation, purification by ion exchange chromatography method with Dowex 1X8 mesh 100-200 as resin was used until obtained 93.26% ± 0.94 of radiochemical purity. Further research is necessary before 131 I-piperine can be used as a radiotracer for cancer diagnosis in nuclear medicine.

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Estimating Binding Capability of Radiopharmaceuticals by Cell Culture Studies

Cited by 5 publications

References 29 publications

Development and radiolabeling of lipid nanoparticles with [99mTc]Tc-HMPAO: Characterization, stability, cytotoxicity and cell binding studies

Development and radiolabeling of lipid nanoparticles with [99mTc]Tc-HMPAO: Characterization, stability, cytotoxicity and cell binding studies

Radiolabeling and In-Silico Study of 131I-(4-fluorobenzoyl-3-methylthiourea) as Radiopharmaceuticals for Breast Cancer Theranostics

Labeling of Piperine with Iodine-131 as Radiotracer in the Development of Cancer Drugs from Indonesia’s Natural Products

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